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. 2007 Mar 15;17(6):1773-8.
doi: 10.1016/j.bmcl.2006.12.077. Epub 2006 Dec 24.

Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2

Yasushi Miyazaki  1 , Jun Tang, Yutaka Maeda, Masato Nakano, Liping Wang, Robert T Nolte, Hideyuki Sato, Masaki Sugai, Yuji Okamoto, Anne T Truesdale, Daniel F Hassler, Eldridge N Nartey, Denis R Patrick, Maureen L Ho, Kazunori Ozawa
Affiliations

Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2

Yasushi Miyazaki et al. Bioorg Med Chem Lett. .

Abstract

During our effort to develop dual VEGFR2 and Tie-2 inhibitors as anti-angiogenic agents for cancer therapy, we discovered 4-amino-5-(4-((2-fluoro-5-(trifluoromethyl)phenyl)- aminocarbonylamino)phenyl)furo[2,3-d]pyrimidine (8a) possessing strong inhibitory activity at both the enzyme and cellular level against VEGFR2 and Tie-2. Compound 8a demonstrated high pharmacokinetic exposure through oral administration, and showed marked tumor growth inhibition and anti-angiogenic activity in mouse HT-29 xenograft model via once-daily oral administration.

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